Sampatrilat is a dual inhibitor of angiotensin converting enzyme (ACE) and neutral endopeptidase (NEP), with potential application as an antihypertensive agent as well as an agent for treatment of congestive heart failure. Because of this unique dual modality, sampatrilat does not cause a sudden and significant drop in blood pressure after administration of the first dose. In addition, sampatrilat and has a much lower propensity to cause common side effects such as dry cough. However, the oral bioavailability of sampatrilat has been reported to be low, as low as 5% in dogs and 2% in man. Clinical pharmacokinetic data show generally low but persistent plasma drug exposure following single and multiple doses.
Consequently, there is a need to provide pharmaceutical formulations which comprise sampatrilat or similar agents that exhibit enhanced oral absorption of the drug and thereby improve its therapeutic efficacy is timely.